国产丙硫氧嘧啶片在中国男性志愿者的人体药动学及生物等效性研究

目的 研究健康男性自愿者口服国产丙硫氧嘧啶片的人体相对生物利用度及生物等效性。方法 20 名健康男性志愿者随机交叉自身对照分别单次口服丙硫氧嘧啶国产及进口片剂各200 mg 。用HPLC 法检测血药浓度,以内标法定量。结果 峰浓度C_max分别为(5.7±1.5)及(5.8±1.8)mg·L^-1;达峰时间T_max分别为(1.4±0.8)及(1.4±0.7)h;消除相半衰期t_1/2分别为(1.7±0.3)及(1.7±0.2)h;AUC_{0 -t}分别为(18.0±4.4)及(17.8±4.6)mg ·h·L^-1;AUC_0-∞分别为(18.1±4.5)及(17.9±4.7)mg·h· L^-1 。受试片相对于参比片的生物利用度为(101.9±13.2)%。结论 丙硫氧嘧啶片国产片和进口片具有生物等效性。

Pharmacokinetics and relative bioavailability of domestic propylthiouracil tablets in Chinese healthy male volunteers

AIM: To study the pharmacokinetics and relative bioavailability of propylthiouracil tablet in Chinese healthy male volunteers.METHODS: The bioequivalence and relative bioavailability of a test domestic formulation of propylthiouracil in comparison with a reference imported formulation was investigated in a randomized 2-way cross-over study in 20 healthy volunteers following a single oral dose of 200 mg.The washout period was 1wk.Plasma concentrations of propylthiouracil were determined by a HPLC system equipped with a ultraviolet detector.RESULTS: The following pharmacokinetical parameters were derived from the individual plasma concentration time courses.The main parameters for test and reference formulations,C_max were(5.7±1.5)and(5.8±1.8)mg·L^-1;t_max were(1.4±0.8)and(1.4±0.7)h;t_1/2were 1.7±0.3 and(1.7±0.2)h;AUC_0-t were(18.0±4.4)and(17.8±4.6)mg·h·L^-1;AUC_0-∞were(18.1±4.5)and(17.9±4.7)mg·h·L^-1,respectively.Compared with reference formulation,the relative bioavailability(F)of test formulation was(101.9±13.2)%。The above parameters obtained from two formulations were compared by analysis of variance(ANOVA)and no significant difference was found.The bioequivalence of two formulations was found assessed by two one-side ways test(p<0.05).CONCLUSION: Therefore,from the results of this study it can be concluded that the test formulation is bioequivalent with the referenceformulation.